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Synthesis and in vitro cytotoxic and antiviral activities of 1-(2,5,6-trideoxy-6-halogenohept-5-enofuranurononitrile)thymine and derivatives
Authors:Tronchet Jean M J  Chalard Frederic  Rivara-Minten Elisabeth  Seman Michel  De Clercq Erik  Balzarini Jan  Dilda Pierre
Affiliation:Department of Organic Pharmaceutical Chemistry, University of Geneva, Sciences II, Switzerland.
Abstract:All 1-(2,5,6-trideoxy-6-halogenohept-5-enofuranurononitrile)thymine and their 3'-O-TBDMS derivatives have been prepared and their configuration established. Some of these compounds are endowed with a cytotoxic or cytostatic activity in cell culture. The single most important factor affecting the cytotoxicity of these compounds is the presence on the molecule of a soft (electrofugal) halogen atom.
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